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PMC12939507
core_pubmed_pmc
Phytochemical Quorum-Sensing Inhibitors Against Bacterial Pathogens: Mechanisms of Action and Translational Challenges
Phytochemical Quorum-Sensing Inhibitors Against Bacterial Pathogens: Mechanisms of Action and Translational Challenges Abstract Abstract Antimicrobial resistance is a critical global health challenge, driven by the rapid emergence of multidrug-resistant bacterial pathogens and exacerbated by extensive antibiotic use, w...
PMC10714423
core_pubmed_pmc
Novel Combination of Erythropoietin and Romiplostim to Treat Chemotherapy-Induced Anemia and Thrombocytopenia via Pharmacodynamic Interaction on Hematopoietic Stem and Progenitor Cells
Novel Combination of Erythropoietin and Romiplostim to Treat Chemotherapy-Induced Anemia and Thrombocytopenia via Pharmacodynamic Interaction on Hematopoietic Stem and Progenitor Cells Abstract Abstract Chemotherapy-induced anemia and thrombocytopenia (CIAT) in cancer patients are often caused by the damage of hematopo...
PMC8721376
core_pubmed_pmc
Tolerance and Pharmacokinetics of Recombinant Human Endostatin Administered as Single-Dose or Multiple-Dose Infusions in Patients With Advanced Solid Tumors: A Phase I Clinical Trial
Tolerance and Pharmacokinetics of Recombinant Human Endostatin Administered as Single-Dose or Multiple-Dose Infusions in Patients With Advanced Solid Tumors: A Phase I Clinical Trial Abstract Objective : This study aimed to investigate the tolerance and pharmacokinetic characteristics of recombinant human endostatin (r...
PMC9078196
core_pubmed_pmc
Quantitative SPECT imaging and biodistribution point to molecular weight independent tumor uptake for some long-circulating polymer nanocarriers
Quantitative SPECT imaging and biodistribution point to molecular weight independent tumor uptake for some long-circulating polymer nanocarriers Abstract Abstract Polymeric nanocarriers are promising entities for cancer diagnosis and therapy. The aim of such nanocarriers is to selectively accumulate in cancerous tissue...
PMC10614995
core_pubmed_pmc
Cerebrospinal Fluid Pharmacokinetics of Nicardipine Following Intrathecal Administration in Subarachnoid Hemorrhage Patients
Cerebrospinal Fluid Pharmacokinetics of Nicardipine Following Intrathecal Administration in Subarachnoid Hemorrhage Patients Abstract Abstract Subarachnoid hemorrhage (SAH) is a devastating type of stroke, leading to high mortality and morbidity rates. Cerebral vasospasm and delayed cerebral ischemia (DCI) are common c...
PMC9931428
core_pubmed_pmc
Rituximab pharmacokinetic and pharmacokinetic–pharmacodynamic evaluation based on a study in diffuse large B‐cell lymphoma: Influence of tumor size on pharmacokinetic and assessment of pharmacokinetic similarity
Rituximab pharmacokinetic and pharmacokinetic–pharmacodynamic evaluation based on a study in diffuse large B‐cell lymphoma: Influence of tumor size on pharmacokinetic and assessment of pharmacokinetic similarity Abstract Abstract Dr. Reddy's Laboratories rituximab (DRL_RI; Dr. Reddy's Laboratories SA, Basel, Switzerlan...
PMC6201813
core_pubmed_pmc
Effects of psoralen on the pharmacokinetics of anastrozole in rats
Effects of psoralen on the pharmacokinetics of anastrozole in rats Abstract Abstract Context: Psoralen and anastrozole are always used together for breast cancer patients in Chinese clinics. Objective: This study investigates the effects of psoralen on the pharmacokinetics of anastrozole in rats and its potential mecha...
PMC5824104
core_pubmed_pmc
Predictive Performance of Physiologically Based Pharmacokinetic Models for the Effect of Food on Oral Drug Absorption: Current Status
Predictive Performance of Physiologically Based Pharmacokinetic Models for the Effect of Food on Oral Drug Absorption: Current Status Abstract A comprehensive search in literature and published US Food and Drug Administration reviews was conducted to assess whether physiologically based pharmacokinetic (PBPK) modeling ...
PMC4658560
core_pubmed_pmc
Assessment of pharmacokinetic compatibility of short acting CDRI candidate trioxane derivative, 99–411, with long acting prescription antimalarials, lumefantrine and piperaquine
Assessment of pharmacokinetic compatibility of short acting CDRI candidate trioxane derivative, 99–411, with long acting prescription antimalarials, lumefantrine and piperaquine Abstract The pharmacokinetic compatibility of short-acting CDRI candidate antimalarial trioxane derivative, 99–411, was tested with long-actin...
PMC12153115
core_pubmed_pmc
Heavy metals and their relationships with lung function and airway inflammation: insights from a population-based study
Heavy metals and their relationships with lung function and airway inflammation: insights from a population-based study Abstract Background Humans are commonly exposed to various heavy metals, but their effects on human respiratory health, especially lung function and airway inflammation, remain poorly understood. Meth...
PMC9540485
core_pubmed_pmc
The Effect of Ibuprofen Exposure and Patient Characteristics on the Closure of the Patent Ductus Arteriosus in Preterm Infants
The Effect of Ibuprofen Exposure and Patient Characteristics on the Closure of the Patent Ductus Arteriosus in Preterm Infants Abstract Abstract Spontaneous closure of the ductus arteriosus depends on gestational age (GA) and might be delayed in preterm infants, resulting in patent ductus arteriosus (PDA). Ibuprofen ca...
PMC11954708
core_pubmed_pmc
Evaluation of Solubility-Limited Absorption as a Surrogate to Predicting Positive Food Effect of BCS II/IV Drugs
Evaluation of Solubility-Limited Absorption as a Surrogate to Predicting Positive Food Effect of BCS II/IV Drugs Abstract Introduction and Objective Physiologically based pharmacokinetic (PBPK) models are increasingly used to predict food effect (FE) but model parameterization is challenged by in vitro–in vivo (IVIV) d...
PMC10966033
core_pubmed_pmc
A CD25-biased interleukin-2 for autoimmune therapy engineered via a semi-synthetic organism
A CD25-biased interleukin-2 for autoimmune therapy engineered via a semi-synthetic organism Abstract Abstract Background Natural cytokines are poorly suited as therapeutics for systemic administration due to suboptimal pharmacological and pharmacokinetic (PK) properties. Recombinant human interleukin-2 (rhIL-2) has sho...
PMC7794391
core_pubmed_pmc
Fibrillar pharmacology of functionalized nanocellulose
Fibrillar pharmacology of functionalized nanocellulose Abstract Cellulose nanocrystals (CNC) are linear organic nanomaterials derived from an abundant naturally occurring biopolymer resource. Strategic modification of the primary and secondary hydroxyl groups on the CNC introduces amine and iodine group substitution, r...
PMC9070572
core_pubmed_pmc
Impact of soft protein interactions on the excretion, extent of receptor occupancy and tumor accumulation of ultrasmall metal nanoparticles: a compartmental model simulation †
Impact of soft protein interactions on the excretion, extent of receptor occupancy and tumor accumulation of ultrasmall metal nanoparticles: a compartmental model simulation † Abstract Ultrasmall metal nanoparticles (NPs) are next-generation nano-based platforms for in vivo disease diagnosis and treatment. Due to their...
PMC4802331
core_pubmed_pmc
The Epidemiologic and Pharmacodynamic Cutoff Values of Tilmicosin against Haemophilus parasuis
The Epidemiologic and Pharmacodynamic Cutoff Values of Tilmicosin against Haemophilus parasuis Abstract The aim of this study was to establish antimicrobial susceptibility breakpoints for tilmicosin against Haemophilus parasuis , which is an important pathogen of respiratory tract infections. The minimum inhibitory con...
PMC12624754
core_pubmed_pmc
Suzetrigine, a Non‐Opioid Small‐Molecule Analgesic: Mechanism of Action, Clinical, and Translational Science
Suzetrigine, a Non‐Opioid Small‐Molecule Analgesic: Mechanism of Action, Clinical, and Translational Science Abstract ABSTRACT The discovery and approval of Suzetrigine (VX‐548, Journavx) marks a significant breakthrough in pain management. It is the first non‐opioid analgesic approved since celecoxib in 1998. Suzetrig...
PMC2992046
core_pubmed_pmc
Novel Method of Monitoring Trace Cytokines and Activated STAT Molecules in the Paws of Arthritic Mice using Multiplex Bead Technology
Novel Method of Monitoring Trace Cytokines and Activated STAT Molecules in the Paws of Arthritic Mice using Multiplex Bead Technology Abstract Abstract Background The use of mouse models to study human disease provides useful data that can provide support for research projects or an existing drug discovery program. How...
PMC9388353
core_pubmed_pmc
Overweight and obesity are not associated with worse clinical outcomes in COVID-19 patients treated with fixed-dose 6 mg dexamethasone
Overweight and obesity are not associated with worse clinical outcomes in COVID-19 patients treated with fixed-dose 6 mg dexamethasone Abstract Abstract Objective A fixed 6 mg dexamethasone dose for 10 days is the standard treatment for all hospitalised COVID-19 patients who require supplemental oxygen. Yet, the pharma...
PMC9520544
core_pubmed_pmc
Glabridin Plays Dual Action to Augment the Efficacy and Attenuate the Hepatotoxicity of Methotrexate in Arthritic Rats
Glabridin Plays Dual Action to Augment the Efficacy and Attenuate the Hepatotoxicity of Methotrexate in Arthritic Rats Abstract Abstract Glabridin is chemically an isoflavane class of natural phenols and is found mainly in the roots of Glycyrrhiza glabra . It has several beneficial pharmacological actions for the manag...
PMC11440962
core_pubmed_pmc
Optimized fosfomycin regimens for treating carbapenem‐resistant Acinetobacter baumannii in critically ill patients with varying degrees of renal function
Optimized fosfomycin regimens for treating carbapenem‐resistant Acinetobacter baumannii in critically ill patients with varying degrees of renal function Abstract Abstract Fosfomycin has been used to treat carbapenem‐resistant Acinetobacter baumannii (CRAB) infections. However, there is insufficient information on dosa...
PMC12297903
core_pubmed_pmc
Pharmacokinetics of Pegaspargase with a Limited Sampling Strategy for Asparaginase Activity Monitoring in Children with Acute Lymphoblastic Leukemia
Pharmacokinetics of Pegaspargase with a Limited Sampling Strategy for Asparaginase Activity Monitoring in Children with Acute Lymphoblastic Leukemia Abstract Background : Asparaginase (ASPase) plays an important role in the therapy of acute lymphoblastic leukemia (ALL). Serum ASPase activity (SAA) can be modified and e...
PMC11062940
core_pubmed_pmc
Pharmacokinetics of isavuconazole at different target sites in healthy volunteers after single and multiple intravenous infusions
Pharmacokinetics of isavuconazole at different target sites in healthy volunteers after single and multiple intravenous infusions Abstract Abstract Background Invasive aspergillosis is a severe fungal infection that affects multiple organ systems including the CNS and the lungs. Isavuconazole, a novel triazole antifung...
PMC8960241
core_pubmed_pmc
Beta-Lactams Therapeutic Monitoring in Septic Children–What Target Are We Aiming for? A Scoping Review
Beta-Lactams Therapeutic Monitoring in Septic Children–What Target Are We Aiming for? A Scoping Review Abstract The antimicrobial therapy of sepsis and septic shock should be individualized based on pharmacokinetic/pharmacodynamic (PK/PD) parameters to deliver effective and timely treatment of life-threatening infectio...
PMC9109144
core_pubmed_pmc
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor Abstract Abstract The nonclassical extracellular signal-related kinase 5 (ERK5) mitogen-activated protein kinase pathway has been implicated in increased cellular proliferation, migration...
PMC5913948
core_pubmed_pmc
Cellular Pharmacokinetics and Intracellular Activity of Gepotidacin against Staphylococcus aureus Isolates with Different Resistance Phenotypes in Models of Cultured Phagocytic Cells
Cellular Pharmacokinetics and Intracellular Activity of Gepotidacin against Staphylococcus aureus Isolates with Different Resistance Phenotypes in Models of Cultured Phagocytic Cells Abstract ABSTRACT Gepotidacin (GSK2140944), a novel triazaacenaphthylene bacterial topoisomerase inhibitor, is currently in clinical deve...
PMC12700429
core_pubmed_pmc
Machine learning-guided identification and simulation-based validation of potent JAK3 inhibitors for cancer therapy
Machine learning-guided identification and simulation-based validation of potent JAK3 inhibitors for cancer therapy Abstract Janus kinase 3 (JAK3) is a hematopoietic-specific kinase implicated in cytokine signaling and immune dysregulation and has recently been associated with cancer progression. However, selective and...
PMC12939157
core_pubmed_pmc
Research Progress on the Anticancer Effect of Ginsenoside Rh1
Research Progress on the Anticancer Effect of Ginsenoside Rh1 Abstract Abstract Cancer is one of the major lethal diseases in the world, and Western medicine treatments are often affected by side effects and drug resistance. Ginseng is a commonly used Chinese medicine in clinical practice, and Ginsenoside Rh1, an impor...
PMC12873072
core_pubmed_pmc
Levels of aripiprazole in the blood with an injection of aripiprazole administered once every two months: a plain language summary of publication
Levels of aripiprazole in the blood with an injection of aripiprazole administered once every two months: a plain language summary of publication Abstract Summary What is this summary about? The information summarized here relates to aripiprazole, a medicine that is used to treat conditions such as schizophrenia and bi...
PMC3417946
core_pubmed_pmc
Review of the efficacy and safety of remifentanil for the prevention and treatment of pain during and after procedures and surgery
Review of the efficacy and safety of remifentanil for the prevention and treatment of pain during and after procedures and surgery Abstract Remifentanil is an ultrashort-acting synthetic opioid. It is metabolized by nonspecific tissue and plasma esterases. Remifentanil’s metabolism is responsible for its unique pharmac...
PMC10202973
core_pubmed_pmc
Potential pharmacological confounders in the setting of death determined by neurologic criteria: a narrative review
Potential pharmacological confounders in the setting of death determined by neurologic criteria: a narrative review Abstract Abstract Guidelines for the determination of death by neurologic criteria (DNC) require an absence of confounding factors if clinical examination alone is to be used. Drugs that depress the centr...
PMC4076844
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic modelling approaches in paediatric infectious diseases and immunology ☆
Pharmacokinetic/pharmacodynamic modelling approaches in paediatric infectious diseases and immunology ☆ Abstract Pharmacokinetic/pharmacodynamic (PKPD) modelling is used to describe and quantify dose–concentration–effect relationships. Within paediatric studies in infectious diseases and immunology these methods are of...
PMC9664866
core_pubmed_pmc
New In Vitro Interaction-Parasite Reduction Ratio Assay for Early Derisk in Clinical Development of Antimalarial Combinations
New In Vitro Interaction-Parasite Reduction Ratio Assay for Early Derisk in Clinical Development of Antimalarial Combinations Abstract ABSTRACT The development and spread of drug-resistant phenotypes substantially threaten malaria control efforts. Combination therapies have the potential to minimize the risk of resista...
PMC5716766
core_pubmed_pmc
Tyrosine kinase inhibitors show different anti-brain metastases efficacy in NSCLC: A direct comparative analysis of icotinib, gefitinib, and erlotinib in a nude mouse model
Tyrosine kinase inhibitors show different anti-brain metastases efficacy in NSCLC: A direct comparative analysis of icotinib, gefitinib, and erlotinib in a nude mouse model Abstract Brain metastasis is an increasing problem in non-small cell lung cancer (NSCLC) patients. Tyrosine kinase inhibitors (TKIs), including gef...
PMC10536547
core_pubmed_pmc
Investigation of the Effect on the Albumin Binding Moiety for the Pharmacokinetic Properties of 68 Ga-, 205/206 Bi-, and 177 Lu-Labeled NAPamide-Based Radiopharmaceuticals
Investigation of the Effect on the Albumin Binding Moiety for the Pharmacokinetic Properties of 68 Ga-, 205/206 Bi-, and 177 Lu-Labeled NAPamide-Based Radiopharmaceuticals Abstract Although radiolabeled alpha-melanocyte stimulating hormone-analogue NAPamide derivatives are valuable melanoma-specific diagnostic probes, ...
PMC12370379
core_pubmed_pmc
Model‐Informed Optimal Dosing of Anti‐ CD47 Antibody Using Target‐Mediated Drug Disposition Model
Model‐Informed Optimal Dosing of Anti‐ CD47 Antibody Using Target‐Mediated Drug Disposition Model Abstract ABSTRACT IMC‐002, an anti‐cluster of differentiation 47 (CD47) antibody, was developed as a fully human immunoglobulin (Ig) G4 monoclonal antibody targeting CD47. IMC‐002 blocks CD47–signal regulatory protein alph...
PMC9138962
core_pubmed_pmc
Evaluation in a Cytokine Storm Model In Vivo of the Safety and Efficacy of Intravenous Administration of PRS CK STORM (Standardized Conditioned Medium Obtained by Coculture of Monocytes and Mesenchymal Stromal Cells)
Evaluation in a Cytokine Storm Model In Vivo of the Safety and Efficacy of Intravenous Administration of PRS CK STORM (Standardized Conditioned Medium Obtained by Coculture of Monocytes and Mesenchymal Stromal Cells) Abstract Our research group has been developing a series of biological drugs produced by coculture tech...
PMC3270437
core_pubmed_pmc
Bayesian Analysis of a Lipid-Based Physiologically Based Toxicokinetic Model for a Mixture of PCBs in Rats
Bayesian Analysis of a Lipid-Based Physiologically Based Toxicokinetic Model for a Mixture of PCBs in Rats Abstract A lipid-based physiologically based toxicokinetic (PBTK) model has been developed for a mixture of six polychlorinated biphenyls (PCBs) in rats. The aim of this study was to apply population Bayesian anal...
PMC9532855
core_pubmed_pmc
Considerations for clinical evaluation of the effects of bariatric surgery on the pharmacokinetics of orally administered drugs
Considerations for clinical evaluation of the effects of bariatric surgery on the pharmacokinetics of orally administered drugs Abstract Abstract Obesity has been a growing worldwide concern, and surgical intervention including bariatric surgery is considered as one of the options for treatment. However, there still is...
PMC10420250
core_pubmed_pmc
Assessment of Purity, Stability, and Pharmacokinetics of NGP-1, a Novel Prodrug of GS441254 with Potential Anti-SARS-CoV-2 Activity, Using Liquid Chromatography
Assessment of Purity, Stability, and Pharmacokinetics of NGP-1, a Novel Prodrug of GS441254 with Potential Anti-SARS-CoV-2 Activity, Using Liquid Chromatography Abstract Abstract SARS-CoV-2 is a highly contagious and pathogenic virus that first appeared in late December 2019 and caused a global pandemic in a short peri...
PMC4573230
core_pubmed_pmc
A Randomized, Double-Blind Pilot Study of Dose Comparison of Ramosetron to Prevent Chemotherapy-Induced Nausea and Vomiting
A Randomized, Double-Blind Pilot Study of Dose Comparison of Ramosetron to Prevent Chemotherapy-Induced Nausea and Vomiting Abstract Abstract Purpose . This study was conducted to determine the optimal dose titration of ramosetron to prevent the Rhodes Index of Nausea, Vomiting, and Retching (RINVR). Methods . Patients...
PMC8327444
core_pubmed_pmc
Pharmacokinetic modeling of over-the-counter drug diphenhydramine self-administered in overdoses in Japanese patients admitted to hospital
Pharmacokinetic modeling of over-the-counter drug diphenhydramine self-administered in overdoses in Japanese patients admitted to hospital Abstract Background Although the over-the-counter H 1 receptor antagonist diphenhydramine is not a common drug of abuse, it was recently recognized as one of the substances causing ...
PMC8202642
core_pubmed_pmc
Setting the Beta-Lactam Therapeutic Range for Critically Ill Patients: Is There a Floor or Even a Ceiling?
Setting the Beta-Lactam Therapeutic Range for Critically Ill Patients: Is There a Floor or Even a Ceiling? Abstract Supplemental Digital Content is available in the text. Keywords: adverse events, antibiotic, intensive care, pharmacodynamics, pharmacokinetics, seizures Abstract OBJECTIVES: Beta-lactam antibiotics exhib...
PMC7322139
core_pubmed_pmc
Remogliflozin Etabonate in the Treatment of Type 2 Diabetes: Design, Development, and Place in Therapy
Remogliflozin Etabonate in the Treatment of Type 2 Diabetes: Design, Development, and Place in Therapy Abstract Abstract Type 2 diabetes mellitus (T2DM) is an emerging epidemic in Asian countries, especially in India. With the advent of the SGLT2 inhibitor class of drugs demonstrating benefits beyond glycemic control, ...
PMC7444351
core_pubmed_pmc
Dynamic contrast-enhanced MRI differentiates hepatocellular carcinoma from hepatic metastasis of rectal cancer by extracting pharmacokinetic parameters and radiomic features
Dynamic contrast-enhanced MRI differentiates hepatocellular carcinoma from hepatic metastasis of rectal cancer by extracting pharmacokinetic parameters and radiomic features Abstract The aim of the present study was to explore how dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) may differentiate hepatoce...
PMC11534100
core_pubmed_pmc
A perioperative study of Safusidenib in patients with IDH1 -mutated glioma
A perioperative study of Safusidenib in patients with IDH1 -mutated glioma Abstract Abstract This is a single arm, open label perioperative trial to assess the feasibility, pharmacokinetics and pharmacodynamics of treatment with safusidenib following biopsy, and prior to surgical resection in patients with IDH1 mutated...
PMC4592215
core_pubmed_pmc
Development of Physiologically Based Pharmacokinetic/Pharmacodynamic Model for Indomethacin Disposition in Pregnancy
Development of Physiologically Based Pharmacokinetic/Pharmacodynamic Model for Indomethacin Disposition in Pregnancy Abstract Abstract Findings of a recent clinical study showed indomethacin has lower plasma levels and higher steady-state apparent clearance in pregnant subjects when compared to those in non-pregnant su...
PMC12655819
core_pubmed_pmc
Volumetric Absorptive Microsampling of Saliva for Pharmacokinetic Evaluation of Mycophenolic Acid and Its Glucuronide Metabolite in Pediatric Renal Transplant Recipients: Bioanalytical Method Validation and Clinical Feasibility Evaluation
Volumetric Absorptive Microsampling of Saliva for Pharmacokinetic Evaluation of Mycophenolic Acid and Its Glucuronide Metabolite in Pediatric Renal Transplant Recipients: Bioanalytical Method Validation and Clinical Feasibility Evaluation Abstract Background: Mycophenolic acid (MPA) is frequently used in pediatric rena...
PMC11798408
core_pubmed_pmc
Protocol of a drug–drug interaction study between bictegravir/emtricitabine/tenofovir alafenamide and feminizing hormones in trans women living with HIV
Protocol of a drug–drug interaction study between bictegravir/emtricitabine/tenofovir alafenamide and feminizing hormones in trans women living with HIV Abstract Abstract Aims: Trans/transfeminine women are disproportionally affected by HIV. Concerns regarding negative drug–drug interactions (DDIs) between ART drugs an...
PMC9095522
core_pubmed_pmc
Biomarkers Predicting Tissue Pharmacokinetics of Antimicrobials in Sepsis: A Review
Biomarkers Predicting Tissue Pharmacokinetics of Antimicrobials in Sepsis: A Review Abstract The pathophysiology of sepsis alters drug pharmacokinetics, resulting in inadequate drug exposure and target-site concentration. Suboptimal exposure leads to treatment failure and the development of antimicrobial resistance. Th...
PMC5686280
core_pubmed_pmc
An automated sampling importance resampling procedure for estimating parameter uncertainty
An automated sampling importance resampling procedure for estimating parameter uncertainty Abstract Abstract Quantifying the uncertainty around endpoints used for decision-making in drug development is essential. In nonlinear mixed-effects models (NLMEM) analysis, this uncertainty is derived from the uncertainty around...
PMC9931436
core_pubmed_pmc
Interspecies and in vitro‐in vivo scaling for quantitative modeling of whole‐body drug pharmacokinetics in patients: Application to the anticancer drug oxaliplatin
Interspecies and in vitro‐in vivo scaling for quantitative modeling of whole‐body drug pharmacokinetics in patients: Application to the anticancer drug oxaliplatin Abstract Abstract Quantitative systems pharmacology holds the promises of integrating results from laboratory animals or in vitro human systems into the des...
PMC6892136
core_pubmed_pmc
Development of a high-precision bladder hyperthermic intracavitary chemotherapy device for bladder cancer and pharmacokinetic study
Development of a high-precision bladder hyperthermic intracavitary chemotherapy device for bladder cancer and pharmacokinetic study Abstract Abstract Background Bladder hyperthermic intracavitary chemotherapy (HIVEC) has good effectiveness for bladder cancer, but conventional HIVEC systems lack precision and convenient...
PMC5836856
core_pubmed_pmc
Thorough QT/QTc Evaluation of the Cardiac Safety of Secnidazole at Therapeutic and Supratherapeutic Doses in Healthy Individuals
Thorough QT/QTc Evaluation of the Cardiac Safety of Secnidazole at Therapeutic and Supratherapeutic Doses in Healthy Individuals Abstract Abstract SYM‐1219, a novel oral granule formulation of secnidazole, is under development as single‐dose treatment for bacterial vaginosis. This 4‐way, randomized, crossover study eva...
PMC7899216
core_pubmed_pmc
Efficacy, Pharmacokinetics, and Safety Over 48 Weeks With Ibalizumab-Based Therapy in Treatment-Experienced Adults Infected With HIV-1: A Phase 2a Study
Efficacy, Pharmacokinetics, and Safety Over 48 Weeks With Ibalizumab-Based Therapy in Treatment-Experienced Adults Infected With HIV-1: A Phase 2a Study Abstract Supplemental Digital Content is Available in the Text. Key Words: ibalizumab, HIV-1, antiretroviral therapy, treatment-experienced, multidrug resistance Abstr...
PMC9764106
core_pubmed_pmc
An innovative ethosuximide granule formulation designed for pediatric use: Comparative pharmacokinetics, safety, tolerability, and palatability profile versus reference syrup
An innovative ethosuximide granule formulation designed for pediatric use: Comparative pharmacokinetics, safety, tolerability, and palatability profile versus reference syrup Abstract Abstract Ethosuximide, the first‐line therapy for childhood absence epilepsy, is currently formulated as a syrup (Zarontin®, Pfizer) wit...
PMC12583984
core_pubmed_pmc
Population Pharmacokinetic and Exposure‐Response Analysis of the Cognitive Effects of TAK‐071 in Participants With Parkinson Disease and Cognitive Impairment
Population Pharmacokinetic and Exposure‐Response Analysis of the Cognitive Effects of TAK‐071 in Participants With Parkinson Disease and Cognitive Impairment Abstract Abstract TAK‐071 is a novel muscarinic M 1 positive allosteric modulator under investigation for the treatment of cognitive impairment and falls associat...
PMC4716585
core_pubmed_pmc
Use of Modeling and Simulation in the Design and Conduct of Pediatric Clinical Trials and the Optimization of Individualized Dosing Regimens
Use of Modeling and Simulation in the Design and Conduct of Pediatric Clinical Trials and the Optimization of Individualized Dosing Regimens Abstract Mathematical models of drug action and disease progression can inform pediatric pharmacotherapy. In this tutorial, we explore the key issues that differentiate pediatric ...
PMC3548122
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of the Proton Pump Inhibitors
Pharmacokinetics and Pharmacodynamics of the Proton Pump Inhibitors Abstract Proton pump inhibitor (PPI) is a prodrug which is activated by acid. Activated PPI binds covalently to the gastric H + , K + -ATPase via disulfide bond. Cys813 is the primary site responsible for the inhibition of acid pump enzyme, where PPIs ...
PMC8990453
core_pubmed_pmc
Safety, tolerability, and efficacy of monoclonal CD38 antibody felzartamab in late antibody-mediated renal allograft rejection: study protocol for a phase 2 trial
Safety, tolerability, and efficacy of monoclonal CD38 antibody felzartamab in late antibody-mediated renal allograft rejection: study protocol for a phase 2 trial Abstract Background Antibody-mediated rejection (ABMR) is a cardinal cause of renal allograft loss. This rejection type, which may occur at any time after tr...
PMC12738542
core_pubmed_pmc
Identification of bioactive phytoconstituents as promising ABL2 inhibitors using virtual screening and molecular dynamics simulation
Identification of bioactive phytoconstituents as promising ABL2 inhibitors using virtual screening and molecular dynamics simulation Abstract ABL proto-oncogene 2 (ABL2) is an essential nonreceptor tyrosine kinase that regulates cytoskeletal dynamics, cell adhesion, and migration. ABL2 is dysregulated in multiple cance...
PMC9968060
core_pubmed_pmc
Chemical and Biological Review of Endophytic Fungi Associated with Morus sp. (Moraceae) and In Silico Study of Their Antidiabetic Potential
Chemical and Biological Review of Endophytic Fungi Associated with Morus sp. (Moraceae) and In Silico Study of Their Antidiabetic Potential Abstract Abstract The chronic nature of diabetes mellitus motivates the quest for novel agents to improve its management. The scarcity and prior uncontrolled utilization of medicin...
PMC6767401
core_pubmed_pmc
Model‐Based Population Pharmacokinetic Analysis of Nivolumab in Chinese Patients With Previously Treated Advanced Solid Tumors, Including Non–Small Cell Lung Cancer
Model‐Based Population Pharmacokinetic Analysis of Nivolumab in Chinese Patients With Previously Treated Advanced Solid Tumors, Including Non–Small Cell Lung Cancer Abstract Abstract Nivolumab is the first anti–programmed death‐1 agent approved in China for treatment of locally advanced or metastatic non–small cell lun...
PMC11150675
core_pubmed_pmc
Simultaneous determination of multiple components in rat plasma by UPLC-MS/MS for pharmacokinetic studies after oral administration of Pogostemon cablin extract
Simultaneous determination of multiple components in rat plasma by UPLC-MS/MS for pharmacokinetic studies after oral administration of Pogostemon cablin extract Abstract Introduction: Pogostemon cablin (PC) is used in traditional Chinese medicine and food, as it exerts pharmacological effects, such as immune-modulatory...
PMC9101911
core_pubmed_pmc
Modeling di (2-ethylhexyl) Phthalate (DEHP) and Its Metabolism in a Body’s Organs and Tissues through Different Intake Pathways into Human Body
Modeling di (2-ethylhexyl) Phthalate (DEHP) and Its Metabolism in a Body’s Organs and Tissues through Different Intake Pathways into Human Body Abstract Phthalate esters (PAEs) are ubiquitous in indoor environments as plasticizers in indoor products. Residences are often exposed to indoor PAEs in the form of gas, parti...
PMC7015735
core_pubmed_pmc
Population pharmacokinetics and pharmacodynamics of dobutamine in neonates on the first days of life
Population pharmacokinetics and pharmacodynamics of dobutamine in neonates on the first days of life Abstract Abstract Aims To describe the pharmacokinetics (PK) and concentration‐related effects of https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=535 in critically ill neonates in the first days o...
PMC8763792
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Based Breakpoints of Polymyxin B for Bloodstream Infections Caused by Multidrug-Resistant Gram-Negative Pathogens
Pharmacokinetic/Pharmacodynamic Based Breakpoints of Polymyxin B for Bloodstream Infections Caused by Multidrug-Resistant Gram-Negative Pathogens Abstract Abstract The latest PK/PD findings have demonstrated negligible efficacy of intravenous polymyxins against pulmonary infections. We investigated pharmacokinetic/phar...
PMC6821876
core_pubmed_pmc
Strategies for Early Prediction and Timely Recognition of Drug-Induced Liver Injury: The Case of Cyclin-Dependent Kinase 4/6 Inhibitors
Strategies for Early Prediction and Timely Recognition of Drug-Induced Liver Injury: The Case of Cyclin-Dependent Kinase 4/6 Inhibitors Abstract The idiosyncratic nature of drug-induced liver injury (DILI) represents a current challenge for drug developers, regulators and clinicians. The myriad of agents (including med...
PMC11578131
core_pubmed_pmc
Informing pregnancy dose via target‐mediated drug disposition modeling and simulations for a recombinant human monoclonal antibody
Informing pregnancy dose via target‐mediated drug disposition modeling and simulations for a recombinant human monoclonal antibody Abstract Abstract RLYB212 is a human monoclonal anti‐human platelet antigen (HPA)‐1a immunoglobulin gamma 1 in clinical development as a subcutaneous injection for the prevention of materna...
PMC11591401
core_pubmed_pmc
Multiple‐dose pharmacokinetics of cenerimod and the effect of charcoal on its elimination
Multiple‐dose pharmacokinetics of cenerimod and the effect of charcoal on its elimination Abstract Abstract Cenerimod is a sphingosine‐1‐phosphate receptor 1 modulator that reduces tissue availability of circulating lymphocytes. The compound is in Phase 3 development for the treatment of systemic lupus erythematosus. I...
PMC9784949
core_pubmed_pmc
Chitosan-Based Gastric Dressing Materials Loaded with Pomegranate Peel as Bioactive Agents: Pharmacokinetics and Effects on Experimentally Induced Gastric Ulcers in Rabbits
Chitosan-Based Gastric Dressing Materials Loaded with Pomegranate Peel as Bioactive Agents: Pharmacokinetics and Effects on Experimentally Induced Gastric Ulcers in Rabbits Abstract This study reported the fabrication and characterization of gastric dressing, composed of gelatine (GEL), chitosan (CH), and pomegranate p...
PMC11226492
core_pubmed_pmc
Beyond nimodipine: advanced neuroprotection strategies for aneurysmal subarachnoid hemorrhage vasospasm and delayed cerebral ischemia
Beyond nimodipine: advanced neuroprotection strategies for aneurysmal subarachnoid hemorrhage vasospasm and delayed cerebral ischemia Abstract The clinical management of aneurysmal subarachnoid hemorrhage (SAH)-associated vasospasm remains a challenge in neurosurgical practice, with its prevention and treatment having ...
PMC4848947
core_pubmed_pmc
Pegylated Trastuzumab Fragments Acquire an Increased in Vivo Stability but Show a Largely Reduced Affinity for the Target Antigen
Pegylated Trastuzumab Fragments Acquire an Increased in Vivo Stability but Show a Largely Reduced Affinity for the Target Antigen Abstract PEGylation of biomolecules is a major approach to increase blood stream half-life, stability and solubility of biotherapeutics and to reduce their immunogenicity, aggregation potent...
PMC8469080
core_pubmed_pmc
Population Pharmacokinetic Analysis of Pazopanib in Patients and Determination of Target AUC
Population Pharmacokinetic Analysis of Pazopanib in Patients and Determination of Target AUC Abstract Abstract Pazopanib is a potent multi-targeted kinase inhibitor approved for the treatment of advanced renal cell carcinoma and soft tissue sarcoma. The pharmacokinetics of pazopanib is characterized by a significant in...
PMC8985535
core_pubmed_pmc
Localization of Multi-Lamellar Vesicle Nanoparticles to Injured Brain Tissue in a Controlled Cortical Impact Injury Model of Traumatic Brain Injury in Rodents
Localization of Multi-Lamellar Vesicle Nanoparticles to Injured Brain Tissue in a Controlled Cortical Impact Injury Model of Traumatic Brain Injury in Rodents Abstract Abstract Severe traumatic brain injury (TBI), such as that suffered by patients with cerebral contusion, is a major cause of death and disability in you...
PMC7496433
core_pubmed_pmc
Pharmacokinetics and Safety of the Novel Selective Progesterone Receptor Modulator Vilaprisan in Participants With Renal Impairment
Pharmacokinetics and Safety of the Novel Selective Progesterone Receptor Modulator Vilaprisan in Participants With Renal Impairment Abstract Abstract This open label, parallel‐group study investigated the pharmacokinetics and safety of a single oral 2‐mg dose of the novel selective progesterone receptor modulator vilap...
PMC8401444
core_pubmed_pmc
Evaluation of Pharmacokinetics and Pharmacodynamics of Deferasirox in Pediatric Patients
Evaluation of Pharmacokinetics and Pharmacodynamics of Deferasirox in Pediatric Patients Abstract Background: Deferasirox (DFX) is commonly used to reduce the chronic iron overload (IO) in pediatric patients. However, the drug is characterized by a large pharmacokinetic variability and approximately 10% of patients may...
PMC10120629
core_pubmed_pmc
Using dynamic oral dosing of rifapentine and rifabutin to simulate exposure profiles of long-acting formulations in a mouse model of tuberculosis preventive therapy
Using dynamic oral dosing of rifapentine and rifabutin to simulate exposure profiles of long-acting formulations in a mouse model of tuberculosis preventive therapy Abstract Administration of tuberculosis preventive therapy (TPT) to individuals with latent tuberculosis infection is an important facet of global tubercul...
PMC5480024
core_pubmed_pmc
Oral Candida in Patients with Fixed Orthodontic Appliance: In Vitro Combination Therapy
Oral Candida in Patients with Fixed Orthodontic Appliance: In Vitro Combination Therapy Abstract Abstract Background Fixed orthodontic appliance (FOA) increases the cariogenic microorganisms of mouth including candida. The aim was to evaluate the pharmacodynamic effects of some antibacterial drugs in combination with m...
PMC6234480
core_pubmed_pmc
Utility of Glycosylated TIMP3 molecules: Inhibition of MMPs and TACE to improve cardiac function in rat myocardial infarct model
Utility of Glycosylated TIMP3 molecules: Inhibition of MMPs and TACE to improve cardiac function in rat myocardial infarct model Abstract Abstract Tissue Inhibitor of Metalloproteinase 3 (TIMP3) is a secreted protein that has a great utility to inhibit elevated metalloproteinase (MMP) activity in injured tissues includ...
PMC12662236
core_pubmed_pmc
Bacteriophage pharmacodynamics studied in an in vitro pharmacokinetic model of infection
Bacteriophage pharmacodynamics studied in an in vitro pharmacokinetic model of infection Abstract Abstract Background Bacteriophage therapy offers an alternative way to counter the menace of increasing antimicrobial resistance. Despite its use in clinical practice for many decades the basic tools to study the translati...
PMC3137651
core_pubmed_pmc
Pharmacodynamic and Pharmacokinetic Interactions of Propranolol with Garlic ( Allium sativum ) in Rats
Pharmacodynamic and Pharmacokinetic Interactions of Propranolol with Garlic ( Allium sativum ) in Rats Abstract Abstract Garlic preparations and propranolol (PRO) are agents recognized as cardioprotective and potent antihypertensive agents when they are used individually. However, there is no report available to explai...
PMC9975127
core_pubmed_pmc
Engineering a modular 44 Ti/ 44 Sc generator: eluate evaluation in preclinical models and estimation of human radiation dosimetry
Engineering a modular 44 Ti/ 44 Sc generator: eluate evaluation in preclinical models and estimation of human radiation dosimetry Abstract Abstract Background 44 Sc/ 47 Sc is an attractive theranostic pair for targeted in vivo positron emission tomographic (PET) imaging and beta-particle treatment of cancer. The 44 Ti/...
PMC4489840
core_pubmed_pmc
Population Pharmacokinetics of an Indian F(ab') 2 Snake Antivenom in Patients with Russell's Viper ( Daboia russelii ) Bites
Population Pharmacokinetics of an Indian F(ab') 2 Snake Antivenom in Patients with Russell's Viper ( Daboia russelii ) Bites Abstract Abstract Background There is limited information on antivenom pharmacokinetics. This study aimed to investigate the pharmacokinetics of an Indian snake antivenom in humans with Russell’s...
PMC6685155
core_pubmed_pmc
Simultaneous UPLC–TQ-MS/MS determination of six active components in rat plasma: application in the pharmacokinetic study of Cyclocarya paliurus leaves
Simultaneous UPLC–TQ-MS/MS determination of six active components in rat plasma: application in the pharmacokinetic study of Cyclocarya paliurus leaves Abstract Abstract Background Cyclocarya paliurus (Batal.) Ijinskaja (CP) is a monotypic genus plant, also called sweet tea tree that belongs to the Juglandaceae family,...
PMC4349992
core_pubmed_pmc
An Enhanced In Vivo Stable Isotope Labeling by Amino Acids in Cell Culture (SILAC) Model for Quantification of Drug Metabolism Enzymes *
An Enhanced In Vivo Stable Isotope Labeling by Amino Acids in Cell Culture (SILAC) Model for Quantification of Drug Metabolism Enzymes * Abstract Many of the enzymes involved in xenobiotic metabolism are maintained at a low basal level and are only synthesized in response to activation of upstream sensor/effector prote...
PMC10946447
core_pubmed_pmc
Lipid-Based Self-Microemulsion of Niclosamide Achieved Enhanced Oral Delivery and Anti-Tumor Efficacy in Orthotopic Patient-Derived Xenograft of Hepatocellular Carcinoma in Mice
Lipid-Based Self-Microemulsion of Niclosamide Achieved Enhanced Oral Delivery and Anti-Tumor Efficacy in Orthotopic Patient-Derived Xenograft of Hepatocellular Carcinoma in Mice Abstract Abstract Introduction We previously identified niclosamide as a promising repurposed drug candidate for hepatocellular carcinoma (HCC...
PMC10723891
core_pubmed_pmc
Impact of Various Estimated Glomerular Filtration Rate Equations on the Pharmacokinetics of Meropenem in Critically Ill Adults
Impact of Various Estimated Glomerular Filtration Rate Equations on the Pharmacokinetics of Meropenem in Critically Ill Adults Abstract Abstract IMPORTANCE: Meropenem dosing is typically guided by creatinine-based estimated glomerular filtration rate (eGFR), but creatinine is a suboptimal GFR marker in the critically i...
PMC2939778
core_pubmed_pmc
Mechanistic modelling of dynamic MRI data predicts that tumour heterogeneity decreases therapeutic response
Mechanistic modelling of dynamic MRI data predicts that tumour heterogeneity decreases therapeutic response Abstract Abstract Background: Dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI) contains crucial information about tumour heterogeneity and the transport limitations that reduce drug efficacy. Mathem...
PMC12526041
core_pubmed_pmc
The novel brain penetrant ataxia-telangiectasia mutated inhibitor WSD0628 provides robust radiosensitization of brain tumor patient-derived xenografts
The novel brain penetrant ataxia-telangiectasia mutated inhibitor WSD0628 provides robust radiosensitization of brain tumor patient-derived xenografts Abstract Abstract Background The ataxia-telangiectasia mutated (ATM) protein coordinates the cellular response to therapeutic radiation, and ATM inhibitors can potential...
PMC9317160
core_pubmed_pmc
Postantifungal Effect of Antifungal Drugs against Candida : What Do We Know and How Can We Apply This Knowledge in the Clinical Setting?
Postantifungal Effect of Antifungal Drugs against Candida : What Do We Know and How Can We Apply This Knowledge in the Clinical Setting? Abstract The study of the pharmacological properties of an antifungal agent integrates the drug pharmacokinetics, the fungal growth inhibition, the fungicidal effect and the postantif...
PMC11576838
core_pubmed_pmc
Physiologically based pharmacokinetic model to predict drug–drug interactions with the antibody–drug conjugate enfortumab vedotin
Physiologically based pharmacokinetic model to predict drug–drug interactions with the antibody–drug conjugate enfortumab vedotin Abstract Enfortumab vedotin is an antibody–drug conjugate (ADC) comprised of a Nectin-4–directed antibody and monomethyl auristatin E (MMAE), which is primarily eliminated through P-glycopro...
PMC9340253
core_pubmed_pmc
Model-Informed Drug Development of New Cefoperazone Sodium and Sulbactam Sodium Combination (3:1): Pharmacokinetic/Pharmacodynamic Analysis and Antibacterial Efficacy Against Enterobacteriaceae
Model-Informed Drug Development of New Cefoperazone Sodium and Sulbactam Sodium Combination (3:1): Pharmacokinetic/Pharmacodynamic Analysis and Antibacterial Efficacy Against Enterobacteriaceae Abstract Objective: Cefoperazone/sulbactam is a commonly used antibiotic combination against the extended-spectrum beta-lactam...
PMC12072072
core_pubmed_pmc
Oleanolic Acid Lactones as Effective Agents in the Combat with Cancers—Cytotoxic and Antioxidant Activity, SAR Analysis, Molecular Docking and ADMETox Profile
Oleanolic Acid Lactones as Effective Agents in the Combat with Cancers—Cytotoxic and Antioxidant Activity, SAR Analysis, Molecular Docking and ADMETox Profile Abstract Abstract Oleanolic acid derivatives, specifically lactones ( 2 – 8 ) and bromolactones ( 9 – 14 ), were synthesised and evaluated for their cytotoxic, a...
PMC5071626
core_pubmed_pmc
Effect of hydrogen bond formation/replacement on solubility characteristics, gastric permeation and pharmacokinetics of curcumin by application of powder solution technology
Effect of hydrogen bond formation/replacement on solubility characteristics, gastric permeation and pharmacokinetics of curcumin by application of powder solution technology Abstract Abstract The present research aimed to improve the dissolution rate and bioavailability of curcumin using the potential of liquisolid tec...
PMC9542014
core_pubmed_pmc
Pharmacokinetics, safety and efficacy of intra‐articular non‐steroidal anti‐inflammatory drug injections for the treatment of osteoarthritis: A narrative review
Pharmacokinetics, safety and efficacy of intra‐articular non‐steroidal anti‐inflammatory drug injections for the treatment of osteoarthritis: A narrative review Abstract Abstract What is known and Objective Osteoarthritis (OA) is a common cause of joint disease and activity limitation in adults. Common therapies to tre...
PMC10837198
core_pubmed_pmc
GPRC5D as a novel target for the treatment of multiple myeloma: a narrative review
GPRC5D as a novel target for the treatment of multiple myeloma: a narrative review Abstract Abstract Multiple myeloma is a genetically complex and heterogenous malignancy with a 5-year survival rate of approximately 60%. Despite advances in therapy, patients experience cycles of remission and relapse, with each success...
PMC4906091
core_pubmed_pmc
Pooled bioequivalence study database from Turkey: characterization of adverse events and determination of split points based on Gini Index as a promising method
Pooled bioequivalence study database from Turkey: characterization of adverse events and determination of split points based on Gini Index as a promising method Abstract Abstract Background Manufacturing of and medication with generic drugs is increasing around the world. Bioequivalence (BE) studies are being performed...
PMC10464192
core_pubmed_pmc
3,3′-Diindolylmethane and indole-3-carbinol: potential therapeutic molecules for cancer chemoprevention and treatment via regulating cellular signaling pathways
3,3′-Diindolylmethane and indole-3-carbinol: potential therapeutic molecules for cancer chemoprevention and treatment via regulating cellular signaling pathways Abstract Abstract Dietary compounds in cancer prevention have gained significant consideration as a viable method. Indole-3-carbinol (I3C) and 3,3′-diindolylme...
PMC11357388
core_pubmed_pmc
Advances in Intrathecal Nanoparticle Delivery: Targeting the Blood–Cerebrospinal Fluid Barrier for Enhanced CNS Drug Delivery
Advances in Intrathecal Nanoparticle Delivery: Targeting the Blood–Cerebrospinal Fluid Barrier for Enhanced CNS Drug Delivery Abstract Abstract The blood–cerebrospinal fluid barrier (BCSFB) tightly regulates molecular exchanges between the bloodstream and cerebrospinal fluid (CSF), creating challenges for effective cen...